Synthesis and Characterization of Related Compounds of Aripiprazole,an Antipsychotic Drug Substance

Three related compounds of aripiprazole were identified during the synthesis. These related compounds were synthesized and characterized by their respective spectral data.     

分裂样精神病和情感性精神障碍患者血清5种元素含量变化的研究

采用原子吸收法测定了分裂样精神病和情感性精神障碍患者血清Ｚｎ，Ｃｕ，Ｆｅ，Ｃａ和Ｍｇ含量。结果表明，分裂样精神病和情感性精神障碍患者血清Ｚｎ和Ｍｇ含量及Ｚｎ／Ｃｕ比值明显低于对照组，而Ｃｕ，Ｆｅ和Ｃａ含量及Ｃａ／Ｍｇ比值明显高于对照组。提示以上５种元素的含量变化与分裂样精神病和情感性精神障碍的发生有关。     

Implications and limitations of cellular reprogramming for psychiatric drug development

Human-induced pluripotent stem cells (hiPSCs) derived from somatic cells of patients have opened possibilities for in vitro modeling of the physiology of neural (and other) cells in psychiatric disease states. Issues in early stages of technology development include (1) establishing a library of cells from adequately phenotyped patients, (2) streamlining laborious, costly hiPSC derivation and characterization, (3) assessing whether mutations or other alterations introduced by reprogramming confound interpretation, (4) developing efficient differentiation strategies to relevant cell types, (5) identifying discernible cellular phenotypes meaningful for cyclic, stress induced or relapsing–remitting diseases, (6) converting phenotypes to screening assays suitable for genome-wide mechanistic studies or large collection compound testing and (7) controlling for variability in relation to disease specificity amidst low sample numbers. Coordination of material for reprogramming from patients well-characterized clinically, genetically and with neuroimaging are beginning, and initial studies have begun to identify cellular phenotypes. Finally, several psychiatric drugs have been found to alter reprogramming efficiency in vitro, suggesting further complexity in applying hiPSCs to psychiatric diseases or that some drugs influence neural differentiation moreso than generally recognized. Despite these challenges, studies utilizing hiPSCs may eventually serve to fill essential niches in the translational pipeline for the discovery of new therapeutics.     

丙泊酚复合司可林在精神病患者无抽搐电休克的应用

目的对丙泊酚复合司可林在精神病患者无抽搐电休克中的应用效果进行分析和总结。方法随机选择江西省新余市第二医院于2014年7月—2016年7月收治的精神科患者140例,均采用无抽搐电休克治疗。所有患者均给予丙泊酚与司可林行麻醉,观察麻醉效果。结果血氧饱和度及血压在给药后、电刺激时及清醒后差异不显著,但电刺激时的心率明显快于给药前,而给药后及清醒后的心率与给药前相比,无显著差异。本组共11例发生不良反应,但程度较轻微,停药后可自行消失,未作特殊处理。结论在精神病患者无抽搐电休克治疗中应用丙泊酚与司可林,心率、血压及血氧饱和度的变化较小,有效性高、安全性好,值得推广。     

Interaction of graphene with antipsychotic drugs: Is there any charge transfer process?

Antipsychotics represent an effective therapy for schizophrenia (a chronic mental disorder). Their benefits are related to the interaction of the drugs with dopamine D2 receptor (D2R). Antipsychotics are classified as agonists or antagonists. One of the working hypotheses is that there is a charge transfer process between the drugs and the receptors, which is different for agonists and antagonists. To have more insight into the nature of the interaction of these molecules and the differences between agonists and antagonists, we analyze the interaction of graphene with three molecules: dopamine, pramipexole (an agonist of dopamine), and risperidone (an antagonist of dopamine). The idea is to use graphene as a simple model to analyze the charge transfer process of these three drugs. Optimized structures, atomic charges, and Density of States results indicate that global charges of dopamine and pramipexole are similar, while for risperidone, it is more than double. Pramipexole is an agonist, and the charge transfer process is similar to that of dopamine. Risperidone is an antagonist, and the charge transfer process is different from dopamine. The charge transfer is more significant with risperidone than with dopamine, and this could be related to the mechanism of action. This is in agreement with the working hypotheses that establish that it is possible to distinguish between agonists and antagonists since they have different capacity to transfer charge.